Preparation of Atorvastatin Pellets and Evaluation of their Physico-Chemical Properties

Abstract

Introduction: Pellets are considered as one of the ideal forms of medicine that have advantages over single form. Including Pellets have high dosage loading capability, have a uniform particle size, are uniformly distributed in the gastrointestinal tract, reduce gastrointestinal stimulation, reduce the risk of a single release of the active substance, produce a steady blood level and decrease the plasma concentration fluctuations. Atorvastatin is a group of statin drugs. Considering that atorvastatin has a low water solubility and high digestive absorption, it is classified as class II drugs. As a result, the bioavailability of this drug is influenced by its low solubility of the drug (12%). Purpose: The purpose of this study was to provide rapid release atorvastatin pellets and evaluate their physicochemical properties. Materials and Methods: The rapid release pellets of this drug were prepared using the Extrusion-Spheronization method. These pellets were prepared using materials such as Avicel, Povidone, Calcium Carbonate, Croscarmellose Sodium, and Myrj52. The particle size of pellets, density, drug content, process efficiency, and disintegration time for all formulations were investigated. Drug release was evaluated from all formulations prepared with the USP II dissolution device. The concentration of atorvastatin calcium in the samples was determined using a UV spectrophotometer at a wavelength of 244 nm. The effect of different disintegrants and surfactants on the preparation of formulations were investigated using data from drug release. Results: The resulting pellets in all formulations had features such as the distribution of narrow particle size, spherical and uniform shape, Bulk density and tape density equals and drug content above 95%. Formulation No.8 had a faster release than other formulations and commercial tablets available on the market.

Conclusion: Using the Extrusion-Spheronization method and Croscarmellose Sodium and Myrj52, we managed to produce fast-release atorvastatin pellets that were faster than commercially available tablets in the market.